Document Detail

PEP8-TAT2, a membrane-permeable peptide, inhibits cyclin-Cdk2 activity in HeLa cells.
MedLine Citation:
PMID:  15327838     Owner:  NLM     Status:  MEDLINE    
Here we show that the PEP8-TAT2 peptide is effectively transduced into HeLa cells and that it inhibits cellular cyclin-Cdk2 activity. Like the PEP8 peptide, the PEP8-TAT2 peptide inhibits Cdk2 activity in vitro with an IC50 value of 5 nM, as determined by an immuno-complex kinase assay. It also inhibits DNA synthesis in and proliferation of cultured HeLa cells by arresting cell cycle at the G1/S transition. Further, the PEP8-TAT2 peptide inhibits cell death-associated Cdk2 activity and thereby prevents apoptotic progression in paclitaxel-treated cells. We propose that this inhibitor peptide is an effective agent to suppress the proliferation of human cancer cells, as well as apoptotic progression, by blocking cellular cyclin-dependent Cdk kinase activity.
Kwang-Hoon Chun; Dae-Kwon Kim; Yun-Won Nam; Seung-Ki Lee
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Cancer letters     Volume:  213     ISSN:  0304-3835     ISO Abbreviation:  Cancer Lett.     Publication Date:  2004 Sep 
Date Detail:
Created Date:  2004-08-25     Completed Date:  2004-11-01     Revised Date:  2012-06-25    
Medline Journal Info:
Nlm Unique ID:  7600053     Medline TA:  Cancer Lett     Country:  Ireland    
Other Details:
Languages:  eng     Pagination:  223-30     Citation Subset:  IM    
Division of Pharmaceutical Biosciences, College of Pharmacy, Seoul National University, 151-742, South Korea.
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MeSH Terms
Amino Acid Transport Systems / chemistry*,  pharmacology*
Antineoplastic Agents, Phytogenic / pharmacology
Apoptosis / drug effects*
Biological Assay
CDC2-CDC28 Kinases / pharmacology*
Carrier Proteins / chemistry*,  pharmacology*
Cell Cycle / drug effects*
Cell Division
Cell Membrane
Cyclin-Dependent Kinase 2
DNA / biosynthesis
HeLa Cells
Paclitaxel / pharmacology
Peptide Fragments / pharmacokinetics,  pharmacology*
Saccharomyces cerevisiae Proteins / chemistry*,  pharmacology*
Vesicular Transport Proteins
Reg. No./Substance:
0/Amino Acid Transport Systems; 0/Antineoplastic Agents, Phytogenic; 0/Carrier Proteins; 0/PEP8 protein, S cerevisiae; 0/Peptide Fragments; 0/Saccharomyces cerevisiae Proteins; 0/TAT2 protein, S cerevisiae; 0/Vesicular Transport Proteins; 33069-62-4/Paclitaxel; 9007-49-2/DNA; EC Kinases; EC protein, human; EC Kinase 2

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